Lomaiviticin A is a complex metabolite with potent cytotoxic anticancer activity. The mechanism of this activity is by virtue of Lomaivitacin A cleaving and intercalating polynucleotides (principally, DNA) and disrupting the cellular processes, especially including cell growth, and selectively producing cancer cell death. Notwithstanding that activity, to date, there has yet to be a therapeutic approach relying on Lomaiviticin A as a cleaving/intercalating agent which delivers/targets these cytotoxic agents to a cancer cell and produces cancer cell death with the level of activity pursuant to the present invention.